Antagonists of the Kv1.5 potassium channel

Amy L. Firth, Jason Yuan

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Potassium channels are an extensive family of ion channels selectively permeable to potassium ions (K+). They serve important functions in many crucial physiological processes and their dysregulation is key in several pathophysiological states, including pulmonary arterial hypertension, cancer and cardiac arrhythmias. One subset of K+ channels is comprised of the voltage-gated K+ (Kv) channels, of which over 40 isoforms have been identified and shown to serve important roles in cellular processes, such as the maintenance of resting membrane potential, cell contractility, neuronal activity and cell proliferation. The Kv1.5 isoform, encoded by the KCNA5 gene, has received much attention, with extensive research already carried out into its physiological, biophysical, structural and molecular properties. It is believed to be a potential target in diseases such as atrial fibrillation and pulmonary hypertension. As a result, a wide variety of pathways and pharmacological tools/drugs with modulatory effects on this channel have been identified. This review focuses on inhibitory regulation of Kv1.5 channels and will outline the following aspects: 1) structure, sequence and function; 2) transcriptional regulation; 3) trafficking; 4) occlusion/inhibition; and 5) altered kinetics or biophysical properties.

Original languageEnglish (US)
Pages (from-to)31-47
Number of pages17
JournalDrugs of the Future
Volume33
Issue number1
DOIs
StatePublished - Jan 2008
Externally publishedYes

Fingerprint

Kv1.5 Potassium Channel
Pulmonary Hypertension
Protein Isoforms
Physiological Phenomena
Voltage-Gated Potassium Channels
Potassium Channels
Ion Channels
Membrane Potentials
Atrial Fibrillation
Cardiac Arrhythmias
Potassium
Maintenance
Cell Proliferation
Pharmacology
Ions
Research
Pharmaceutical Preparations
Genes
Neoplasms

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

Cite this

Antagonists of the Kv1.5 potassium channel. / Firth, Amy L.; Yuan, Jason.

In: Drugs of the Future, Vol. 33, No. 1, 01.2008, p. 31-47.

Research output: Contribution to journalArticle

Firth, Amy L. ; Yuan, Jason. / Antagonists of the Kv1.5 potassium channel. In: Drugs of the Future. 2008 ; Vol. 33, No. 1. pp. 31-47.
@article{58f58add3a4546938c159a012a89f076,
title = "Antagonists of the Kv1.5 potassium channel",
abstract = "Potassium channels are an extensive family of ion channels selectively permeable to potassium ions (K+). They serve important functions in many crucial physiological processes and their dysregulation is key in several pathophysiological states, including pulmonary arterial hypertension, cancer and cardiac arrhythmias. One subset of K+ channels is comprised of the voltage-gated K+ (Kv) channels, of which over 40 isoforms have been identified and shown to serve important roles in cellular processes, such as the maintenance of resting membrane potential, cell contractility, neuronal activity and cell proliferation. The Kv1.5 isoform, encoded by the KCNA5 gene, has received much attention, with extensive research already carried out into its physiological, biophysical, structural and molecular properties. It is believed to be a potential target in diseases such as atrial fibrillation and pulmonary hypertension. As a result, a wide variety of pathways and pharmacological tools/drugs with modulatory effects on this channel have been identified. This review focuses on inhibitory regulation of Kv1.5 channels and will outline the following aspects: 1) structure, sequence and function; 2) transcriptional regulation; 3) trafficking; 4) occlusion/inhibition; and 5) altered kinetics or biophysical properties.",
author = "Firth, {Amy L.} and Jason Yuan",
year = "2008",
month = "1",
doi = "10.1358/dof.2008.033.01.1177607",
language = "English (US)",
volume = "33",
pages = "31--47",
journal = "Drugs of the Future",
issn = "0377-8282",
publisher = "Prous Science",
number = "1",

}

TY - JOUR

T1 - Antagonists of the Kv1.5 potassium channel

AU - Firth, Amy L.

AU - Yuan, Jason

PY - 2008/1

Y1 - 2008/1

N2 - Potassium channels are an extensive family of ion channels selectively permeable to potassium ions (K+). They serve important functions in many crucial physiological processes and their dysregulation is key in several pathophysiological states, including pulmonary arterial hypertension, cancer and cardiac arrhythmias. One subset of K+ channels is comprised of the voltage-gated K+ (Kv) channels, of which over 40 isoforms have been identified and shown to serve important roles in cellular processes, such as the maintenance of resting membrane potential, cell contractility, neuronal activity and cell proliferation. The Kv1.5 isoform, encoded by the KCNA5 gene, has received much attention, with extensive research already carried out into its physiological, biophysical, structural and molecular properties. It is believed to be a potential target in diseases such as atrial fibrillation and pulmonary hypertension. As a result, a wide variety of pathways and pharmacological tools/drugs with modulatory effects on this channel have been identified. This review focuses on inhibitory regulation of Kv1.5 channels and will outline the following aspects: 1) structure, sequence and function; 2) transcriptional regulation; 3) trafficking; 4) occlusion/inhibition; and 5) altered kinetics or biophysical properties.

AB - Potassium channels are an extensive family of ion channels selectively permeable to potassium ions (K+). They serve important functions in many crucial physiological processes and their dysregulation is key in several pathophysiological states, including pulmonary arterial hypertension, cancer and cardiac arrhythmias. One subset of K+ channels is comprised of the voltage-gated K+ (Kv) channels, of which over 40 isoforms have been identified and shown to serve important roles in cellular processes, such as the maintenance of resting membrane potential, cell contractility, neuronal activity and cell proliferation. The Kv1.5 isoform, encoded by the KCNA5 gene, has received much attention, with extensive research already carried out into its physiological, biophysical, structural and molecular properties. It is believed to be a potential target in diseases such as atrial fibrillation and pulmonary hypertension. As a result, a wide variety of pathways and pharmacological tools/drugs with modulatory effects on this channel have been identified. This review focuses on inhibitory regulation of Kv1.5 channels and will outline the following aspects: 1) structure, sequence and function; 2) transcriptional regulation; 3) trafficking; 4) occlusion/inhibition; and 5) altered kinetics or biophysical properties.

UR - http://www.scopus.com/inward/record.url?scp=41049117740&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=41049117740&partnerID=8YFLogxK

U2 - 10.1358/dof.2008.033.01.1177607

DO - 10.1358/dof.2008.033.01.1177607

M3 - Article

VL - 33

SP - 31

EP - 47

JO - Drugs of the Future

JF - Drugs of the Future

SN - 0377-8282

IS - 1

ER -